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The successful application of synthetic organic chemistry to the biotherapeutic arena has created an exciting paradigm for drug discovery and new opportunities for medicinal chemistry design. Chemistry is no longer restricted to the discovery of small molecule organic drugs since the workable opportunity space is arguably the entire spectrum of chemical space, inclusive of inorganics and biomolecules. Moreover, the emphasis for biotherapeutics is increasingly becoming the alignment of structure with function, and therefore methods that enable the delineation of structure-function relationships will become powerful tools in the design of improved therapeutics, thus avoiding traditionally empirical approaches. Chemistry can significantly modify the structure of a biological, improving its therapeutic effectiveness or imparting totally new properties to the designed molecule, thereby increasing the functionality of the construct. Here, the recent advances made in the area of chemistry-enabled biotherapeutics, or chemologics, are reviewed with a focus on the opportunities being unearthed through close partnerships between biology and chemistry.

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